GKT137831 is primarily used in research settings as a dual inhibitor of NADPH oxidase (NOX) enzymes, specifically targeting NOX1 and NOX4 isoforms. These enzymes are involved in the production of reactive oxygen species (ROS), which play a role in oxidative stress and inflammation. Due to this mechanism, GKT137831 has been investigated for its potential therapeutic effects in various disease models. It has shown promise in preclinical studies related to fibrotic diseases, including liver and kidney fibrosis, where excessive ROS contribute to tissue damage and scarring. In models of diabetic nephropathy, GKT137831 helps reduce inflammation, oxidative stress, and extracellular matrix accumulation, thereby preserving organ function. The compound is also explored in cardiovascular research, particularly in hypertension and vascular remodeling, where NOX-derived ROS are implicated in endothelial dysfunction and arterial stiffness. Additionally, studies in pulmonary hypertension and cancer have evaluated GKT137831 for its ability to modulate tumor microenvironment and reduce fibrosis-related signaling. Overall, GKT137831 serves as a valuable tool compound for understanding the role of NOX enzymes in disease and supports the development of targeted therapies for conditions driven by oxidative stress and chronic inflammation.